APETx2

APETx2 is selective and reversible blocker of acid-sensing ion channel 3 (ASIC3) (ic50 values are 63 and 175 nm for homomeric rat and human asic3 channels). It also inhibits nav1.8 and nav1.2 channels (ic50 values are 55 and 114 nm respectively). It shows analgesic effect on acid induced and inflammatory pain.

Please kindly note that our products and services can only be used to support research purposes (Not for clinical use).
APETx2(CAS 713544-47-9)

CAT No: R0883

CAS No: 713544-47-9

Quick InquiryCustom Peptide Synthesis

cGMP Peptide

Registration of APIs CMC information required for an IND

IND and NDA support Drug master files (DMF) filing

Synonyms/AliasAPETx2;713544-47-9;H-Gly-DL-xiThr-DL-Ala-DL-Cys(1)-DL-Ser-DL-Cys(2)-Gly-DL-Asn-DL-Ser-DL-Lys-Gly-DL-xiIle-DL-Tyr-DL-Trp-DL-Phe-DL-Tyr-DL-Arg-DL-Pro-DL-Ser-DL-Cys(3)-DL-Pro-DL-xiThr-DL-Asp-DL-Arg-Gly-DL-Tyr-DL-xiThr-Gly-DL-Ser-DL-Cys(2)-DL-Arg-DL-Tyr-DL-Phe-DL-Leu-Gly-DL-xiThr-DL-Cys(1)-DL-Cys(3)-DL-xiThr-DL-Pro-DL-Ala-DL-Asp-OH;APETx2 TFA;APE-4472-S;NDB54447;AKOS024458355;DA-70987;Gly-Thr-Ala-Cys-Ser-Cys-Gly-Asn-Ser-Lys-Gly-Ile-Tyr-Trp-Phe-Tyr-Arg-Pro-Ser-Cys-Pro-Thr-Asp-Arg-Gly-Tyr-Thr-Gly-Ser-Cys-Arg-Tyr-Phe- Leu-Gly-Thr-Cys-Cys-Thr-Pro-Ala-Asp;
M.F/FormulaC196H280N54O61S6
M.W/Mr.4561
SequenceOne Letter Code:GXACSCGNSKGXYWFYRPSCPXDRGYXGSCRYFLGXCCXPAD
Three Letter Code:H-Gly-DL-xiThr-DL-Ala-DL-Cys(1)-DL-Ser-DL-Cys(2)-Gly-DL-Asn-DL-Ser-DL-Lys-Gly-DL-xiIle-DL-Tyr-DL-Trp-DL-Phe-DL-Tyr-DL-Arg-DL-Pro-DL-Ser-DL-Cys(3)-DL-Pro-DL-xiThr-DL-Asp-DL-Arg-Gly-DL-Tyr-DL-xiThr-Gly-DL-Ser-DL-Cys(2)-DL-Arg-DL-Tyr-DL-Phe-DL-Leu-Gly-DL-xiThr-DL-Cys(1)-DL-Cys(3)-DL-xiThr-DL-Pro-DL-Ala-DL-Asp-OH
Labeling TargetAcid-sensing ion channel 3 (ASIC3)
Purity>98%
ActivityBlocker
Source#Synthetic
Solubility-20 °C
InChIInChI=1S/C196H280N54O61S6/c1-12-94(4)152-186(303)230-125(71-107-48-56-112(263)57-49-107)169(286)229-126(72-108-77-209-114-34-20-19-33-113(108)114)170(287)228-122(67-103-31-17-14-18-32-103)167(284)227-123(69-105-44-52-110(261)53-45-105)165(282)223-118(38-25-61-208-196(204)205)190(307)248-62-26-40-141(248)183(300)235-133(86-254)177(294)241-139-92-317-316-91-138(181(298)247-157(101(11)259)192(309)250-64-28-39-140(250)182(299)215-95(5)158(275)232-129(193(310)311)75-151(273)274)239-180(297)137-90-315-313-88-135(236-159(276)96(6)216-187(304)154(98(8)256)242-144(265)76-198)179(296)234-132(85-253)176(293)237-134(163(280)213-79-146(267)218-127(73-143(199)264)171(288)233-131(84-252)175(292)221-115(35-21-22-58-197)160(277)211-81-148(269)243-152)87-312-314-89-136(178(295)222-117(37-24-60-207-195(202)203)164(281)225-124(70-106-46-54-111(262)55-47-106)168(285)226-121(66-102-29-15-13-16-30-102)166(283)224-119(65-93(2)3)162(279)212-82-149(270)244-155(99(9)257)188(305)240-137)238-174(291)130(83-251)219-147(268)80-214-185(302)153(97(7)255)245-173(290)120(68-104-42-50-109(260)51-43-104)217-145(266)78-210-161(278)116(36-23-59-206-194(200)201)220-172(289)128(74-150(271)272)231-189(306)156(100(10)258)246-184(301)142-41-27-63-249(142)191(139)308/h13-20,29-34,42-57,77,93-101,115-142,152-157,209,251-263H,12,21-28,35-41,58-76,78-92,197-198H2,1-11H3,(H2,199,264)(H,210,278)(H,211,277)(H,212,279)(H,213,280)(H,214,302)(H,215,299)(H,216,304)(H,217,266)(H,218,267)(H,219,268)(H,220,289)(H,221,292)(H,222,295)(H,223,282)(H,224,283)(H,225,281)(H,226,285)(H,227,284)(H,228,287)(H,229,286)(H,230,303)(H,231,306)(H,232,275)(H,233,288)(H,234,296)(H,235,300)(H,236,276)(H,237,293)(H,238,291)(H,239,297)(H,240,305)(H,241,294)(H,242,265)(H,243,269)(H,244,270)(H,245,290)(H,246,301)(H,247,298)(H,271,272)(H,273,274)(H,310,311)(H4,200,201,206)(H4,202,203,207)(H4,204,205,208)
InChI KeyHEHYILNFEUDIQC-UHFFFAOYSA-N
References

The structural characteristics of APETx2 are compared with that of PcTx1, another effector of ASIC channels but specific to the ASIC1a subtype and to APETx1, a toxin structurally related to APETx2, which targets the HERG potassium channel.

Solution structure of APETx2, a specific peptide inhibitor of ASIC3 proton-gated channels

ASICs appear to be key mediators of inflammatory pain. ASIC antagonists and antisense oligonucleotides reduced both thermal and mechanical hyperalgesia in a rat model of inflammatory pain, highlighting the utility of selective pharmacological agents for studying ASIC channel function. Unfortunately, only two selective ASIC inhibitors have been discovered. The tarantula toxin PcTx1 is a specific blocker of homomeric ASIC1a channels, whereas the sea anemone peptide APETx2 blocks homomeric ASIC3 and ASIC3-containing heteromeric channels. PcTx1 is potently analgesic in mouse models of inflammatory and neuropathic pain, while APETx2 abolishes acid-induced pain in rats. Thus, APETx2 is an invaluable tool for study of ASIC3 channels.

Chemical synthesis and folding of APETx2, a potent and selective inhibitor of acid sensing ion channel 3

Write a review Ask a question
My Review for APETx2

Required fields are marked with *

  • Basic Information
×
Ask a Question for APETx2

Required fields are marked with *

  • Basic Information
×
Useful Tools

Peptide Calculator

Abbreviation List

Peptide Glossary

If you have any peptide synthesis requirement in mind, please do not hesitate to contact us. We will endeavor to provide highly satisfying products and services.

Featured Services
Hot Products
  • Fertirelin Acetate

    Fertirelin acetate is a potent LHRH agonist. After a transient increase, continuous administration results in downregulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis.

    Inquiry
  • Gonadorelin Acetate

    Gonadorelin is a trophic peptide hormone responsible for the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary. GnRH is synthesized and released from GnRH neurons within the hypothalamus. The peptide belongs to gonadotropin-releasing hormone family. It constitutes the initial step in the hypothalamic–pituitary–gonadal axis.

    Inquiry
  • Glucagon

    Glucagon (Porcine glucagon) is a peptide hormone, produced by pancreatic α-cells. Glucagon stimulates gluconeogenesis. Glucagon decreases the activity of HNF-4. Glucagon increases HNF4α phosphorylation.

    Inquiry
  • Alarelin acetate

    Alarelin acetate is a synthetic LH-RH agonist, and stimulates the release of FSH and LH from the pituitary gland. It is known for its induction of ovulation and used to treat endmometriosis.

    Inquiry
  • Angiotensin II Acetate

    Angiotensin II is an octapeptide that produced from angiotensin I after the removal of two amino acids at the C-terminal by angiotensin-converting enzyme (ACE). Angiotensin II is mediated by AT1 and AT2 receptors, which are seven transmembrane glycoproteins with 30% sequence similarity.

    Inquiry
  • Icatibant

    Icatibant (Firazyr) is a synthetic peptidomimetic drug consisting of ten amino acids, and acts as an effective and specific antagonist of bradykinin B2 receptors. It has been approved in the EU for use in hereditary angioedema, and is under investigation for a number of other conditions in which bradykinin is thought to play a significant role.

    Inquiry
  • GLP-1 (7-37) Acetate

    Glucagon-like peptide-1 (GLP-1) is an incretin derived from the transcription product of the proglucagon gene. The major source of GLP-1 in the body is the intestinal L cell that secretes GLP-2 as a gut hormone.

    Inquiry
  • Carbetocin

    Carbetocin is a long-acting synthetic agonist analogue of human oxytocin, with antihemorrhagic and uterotonic activities. Upon administration, carbetocin targets, binds to and activates peripheral oxytocin receptors that are present on the smooth musculature of the uterus. This causes uterus contractions and prevents excessive bleeding after childbirth, particularly following Cesarean section, and may be used to decrease blood loss during hysteroscopic myomectomy.

    Inquiry
  • Thymosin β4 Acetate

    Thymosin β4 is a 43 amino acid peptide which is regarded as the main intracellular G-actin sequestering peptide. Extracellular thymosin β4 may contribute to physiological processes such as angiogenesis, wound healing and regulation of inflammation.

    Inquiry
  • Atosiban

    Atosiban is a nonapeptide, desamino-oxytocin analogue, and a competitive vasopressin/oxytocin receptor antagonist (VOTra). Atosiban is indicated to delay imminent pre-term birth in pregnant adult women. Atosiban is useful in improving the pregnancy outcome of in vitro fertilization-embryo transfer (IVF-ET) in patients with repeated implantation failure (RIF). The pregnancy rate improved from zero to 43.7%.

    Inquiry
Get in touch with us

Copyright © 2025 Creative Peptides. All rights reserved.